< GPCR News < GPCRs in Oncology and Immunology Chemokine Physiology in Cancer Published date November In cancer, chemokines play paradoxical roles in both the directed emigration of metastatic, receptor-expressing cancer cells out of the tumor as well as immigration of tumor infiltrating immune cells that culminate Facets of chemokine physiology across discrete cancer immune phenotypes are contrasted to existing chemokine-centered therapies in cancer.

< GPCR News < GPCRs in Oncology and Immunology Biochemical pharmacology of adenylyl cyclases in cancer date October 1, 2024 Abstract "Globally, despite extensive research and pharmacological advancement, cancer Understanding the signaling pathways involved in cancer progression is essential for the discovery of The expression patterns of ACs in numerous cancers are discussed. , G protein , GPCR , Hallmarks of Cancer , cAMP signaling .

< GPCR News < GPCRs in Oncology and Immunology GPR176 Promotes Cancer Progression by Interacting with G Protein GNAS to Restrain Cell Mitophagy in Colorectal Cancer Published date March 11, 2023 Abstract belongs to the G protein-coupled receptor superfamily, which responds to external stimuli and regulates cancer progression, but its role in colorectal cancer (CRC) remains unclear. In the present study, expression analyses of GPR176 are performed in patients with colorectal cancer.

< GPCR News < GPCRs in Oncology and Immunology The landscape of cancer-rewired GPCR signaling axes Published 2024 Abstract "We explored the dysregulation of G-protein-coupled receptor (GPCR) ligand systems in cancer Multiple GPCRs are differentially regulated together with their upstream partners across cancer subtypes Remarkably, we identified many such axes across several cancer molecular subtypes, including many involving , cancer cell lines , cell-cell communication , drug repurposing , personalized medicine , signaling

< GPCR News < GPCRs in Oncology and Immunology Role and recent progress of P2Y12 receptor in cancer development P2Y12R activation can promote platelet aggregation and adhesion to cancer cells, promote tumor angiogenesis immune microenvironment (TIME) and tumor drug resistance, which is conducive to the progression of cancers cancer. However, a new study suggests that long-term use of P2Y12R inhibitors may increase the risk of cancer

Immunology Involvement of Protease-Activated Receptor2 Pleckstrin Homology Binding Domain in Ovarian Cancer Fallopian Tubes and Drug Design Published date January 22, 2024 Abstract "Studying primordial events in cancer While the involvement of G-protein-coupled receptors (GPCRs) in cancer is growing, GPCR-based therapies PAR2 expression in FTs may serve as an early prediction sensor for ovarian cancer. serve as a powerful medicament in STICs and ovarian cancer.

GPCR News < GPCRs in Oncology and Immunology From odor to oncology: non-canonical odorant receptors in cancer sensory perception, emerging evidence suggests a compelling interplay between odorant receptors and cancer types, suggesting their contributions to cancer progression. The roles of these non-canonical chemoreceptors in cancer are complex, with some receptors promoting tumorigenesis and others acting as tumor-suppressing factors upon activation, depending on the cancer

to schedule Inhibition of Relaxin Autocrine Signaling Confers Therapeutic Vulnerability in Ovarian Cancer Rottapel is a Senior Scientist at the Princess Margaret Cancer Centre where he holds the Amgen Chair for Cancer Research. Rottapel’s research interests lies in the elucidation of signal transduction pathways in cancer, immune He has focussed on developing a comprehensive map of ovarian cancer essential genes using whole genome

Minireview: functional roles of tissue kallikrein, kinins, and kallikrein-related peptidases in lung cancer Published date July 3, 2023 Abstract "Despite campaigns and improvements in detection and treatment, lung cancer One approach to treating patients suffering from lung cancer is to target surface receptors overexpressed , such as prostate and ovarian cancer, facilitating the invasive and metastatic capacity of tumor cells Since lung cancer is often diagnosed in advanced stages, our efforts should focus on early diagnosis,

and Immunology Mechanistic exploration of bioactive constituents in Gnetum gnemon for GPCR-related cancer integral membrane proteins that have gained considerable attention as drug targets, particularly in cancer Gnetum gnemon (GG) for the development of of pharmaceuticals targeting GPCRs within the context of cancer We retrieved targets for GG-derived compounds and GPCRs-related cancer from databases. Survival analysis established the clinical prognostic relevance of identified hub genes in cancer.

Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule G Proteins and GPCRs in Cancer Department of Pharmacology, School of Medicine, and Associate Director for Basic Science at the Moores Cancer treatments, and to identify novel multimodal strategies to enhance the response to cancer immunotherapies Silvio Gutkind on the web Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications Pubmed LinkedIn Twitter UCSD Moores Cancer Center Dr.

< GPCR News < GPCRs in Oncology and Immunology Ultrasensitive dose-response for asbestos cancer risk is expected for damage that accumulates in proportion to dose, as hypothesized for increased risk of cancer relation to genotoxic dose according to the multistage somatic mutation/clonal-expansion theory of cancer Mesothelioma and lung cancer induced by exposure to carcinogenic (e.g., certain asbestos) fibers in humans A recent Inflammation Somatic Mutation (ISM) theory of cancer posits instead that tissue-damage-associated

< GPCR News < GPCRs in Oncology and Immunology Pan-cancer functional analysis of somatic mutations in GPCRs) are the most frequently exploited drug target family, moreover they are often found mutated in cancer We explored cancer-related mutation patterns in all GPCR classes combined and individually. A Two-Entropy Analysis confirmed the correlation between residue conservation and cancer-related mutation families, but also discovered novel GPCRs which had not been linked to cancer before such as the P2Y

GPCRs in Oncology and Immunology Unveiling G-protein coupled receptors as potential targets for ovarian cancer analysis to in vitro validation Published date July 27, 2024 Abstract "Genetic heterogeneity in ovarian cancer To address the genetic heterogeneity of ovarian cancer, a future personalised approach could include the identification of unique GPCRs expressed in cancer biopsies, matched with personalised GPCR-targeted Subsequently, primary ovarian cancer cells derived from ascites and ovarian cancer cell lines were used

< GPCR News < GPCRs in Oncology and Immunology Lactate receptor GPR81 drives breast cancer growth and DLL4 Published date November 22, 2023 Abstract " Background: The lactate receptor GPR81 contributes to cancer Here, we investigate the roles of GPR81 in three-dimensional (3D) and in vivo growth of breast cancer Methods: GPR81 was stably knocked down (KD) in MCF-7 human breast cancer cells which were subjected to lactate and 3D growth in breast cancer spheroids.

coupled receptors (GPCRs) in breast cancer, and his interest in pancreatic cancer. as a potential drug target due to its high expression in triple negative breast cancer. Mike then transitioned to pancreatic cancer, questioning why genes are dysregulated in cancer, which led him to explore different aspects of gene regulation and its relation to cancer progression. fibroblasts and is crucial for their function, leading to complications in cancer patients.

Deciphering a GPCR-lncRNA-miRNA Nexus: Identification of an Aberrant Therapeutic Target in Ovarian Cancer Published date April 18, 2024 Abstract "Ovarian cancer ranks as a leading cause of mortality among gynecological Previous studies have identified the pivotal role of Lysophosphatidic acid (LPA)-signaling in ovarian cancer UCA1 expression inversely correlates with survival outcomes and therapy response in ovarian cancer clinical xenografts, demonstrating the therapeutic potential of targeting LPAR-UCA1-let-7 axis in ovarian cancer

and Immunology Investigating isoform switching in RHBDF2 and its role in neoplastic growth in breast cancer Published date November 1, 2022 Abstract Background: Breast cancer is the second leading cause of cancer-related In the past, studies predicting therapeutic drug targets for cancer therapy focused on the assumption Therefore, there is always an immense need to find promising and novel anti-cancer drug targets. Tags Breast cancer; EGFR; ERAD; RHBDF2; TACE; iRhom2.

Immunology Pharmacological inhibition of neuropeptide Y receptors Y1 and Y5 reduces hypoxic breast cancer This abundance is exploited for cancer imaging, but there is interest in pharmacological inhibition of the NPYRs to interrogate their functional relevance in breast cancer. Therefore, these antagonists may aid in the development of novel cancer therapeutics and patient-based Tags Breast cancer , GPCR , Hypoxia , NPY , Neuropeptide .

Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer and is involved in several cancer phenotypes including tumor growth, survival, and metastasis. The roles of histamine and histamine receptor H1 (HRH1) in cancer pathogenesis remain controversial. Here, we show that HRH1 is widely expressed in various cancer cell lines and cancer tissues and that coexpression of CXCR4 and HRH1 is associated with poor prognosis in breast cancer.

Metallo-protease Peptidase M84 from Bacillusaltitudinis induces ROS-dependent apoptosis in ovarian cancer had no discernible impact on normal cell survival, but it specifically induced apoptosis in ovarian cancer PAR-1, a GPCR which is reported to be overexpressed in ovarian cancer cells, was identified as a target This evoked apoptotic death of the ovarian cancer cells through the intrinsic route. This established Peptidase M84 as a drug candidate for receptor mediated targeted-therapy of ovarian cancer

News < GPCRs in Oncology and Immunology Agonists of galanin subtype 2 receptor may prevent pancreatic cancer and agonists of angiotensin II type 2 receptor may prevent colorectal cancer Published date June 24, of colorectal carcinoma (CRC) is better than that of PDAC, it still is the second-leading cause of cancer receptor inhibited the growth of GAL2 receptor-expressing patient-derived xenografts (PDX) of pancreatic cancer lanthionine-constrained agonist of angiotensin II type 2 (AT2) receptor inhibited PDX of colorectal cancer

< GPCRs in Oncology and Immunology GPR143 controls ESCRT-dependent exosome biogenesis and promotes cancer GPR143 is elevated in multiple cancers, and quantitative proteomic and RNA profiling of exosomes in human cancer cell lines showed that the GPR143-ESCRT pathway promotes secretion of exosomes that carry unique findings provide a mechanism for regulating the exosomal proteome and demonstrate its ability to promote cancer , Sun-Young Kong , Taejoon Kwon , Pann-Ghill Suh , Young Chan Chae Tags GPR143 , HRS , MVB , breast cancer

< GPCR News < GPCRs in Oncology and Immunology Molecular characterization of breast cancer cell pools Abstract "Background: About one-third of patients with estrogen receptor alpha (ERα)-positive breast cancer PR is an important prognostic factor in breast cancer. New evidence has shown that progesterone (P4) has an anti-proliferative effect in ERα-positive breast cancer However, the role of PR in breast cancer is only poorly understood.

< GPCR News < GPCRs in Oncology and Immunology Functional Assessment of Cancer-Linked Mutations in Sensitive Genetic variants in RGS proteins are associated with many diseases, including cancers, although the impact Intolerant and tolerant-control residues that overlap with pathogenic cancer mutations reported in the COSMIC cancer database were selected to define the functional phenotype. Identified intolerant residues with reported cancer-linked mutations RGS14-R173C/H and RGS4-K125Q/E126K

Expanding role of CXCR2 and therapeutic potential of CXCR2 antagonists in inflammatory diseases and cancers is G protein-coupled receptor (GPCR) and plays important roles in various inflammatory diseases and cancers , including chronic obstructive pulmonary disease (COPD), atherosclerosis, asthma, and pancreatic cancer structure-activity relationships and clinical significance of CXCR2 antagonists in inflammatory diseases and cancers Authors Yishi Xie , Wenbin Kuang , Dawei Wang , Kai Yuan , Peng Yang Tags CXCR2 , CXCR2 antagonist , Cancer

< GPCR News < GPCRs in Oncology and Immunology The Effect of Cancer-Associated Mutations on Ligand Binding regulating mood, appetite, and reproductive behavior, it has been identified as a potential target for cancer In this study, we aimed to investigate the effects of cancer patient-derived 5-HT2C receptor mutations sequencing data from the Genomic Data Commons data portal (GDC), we selected 12 mutations from multiple cancer P van Westen, Erik H J Danen, Laura H Heitman Tags 5-HT(2C) receptor , G protein-coupled receptor , cancer

A large component of his work is centered around dysregulated signaling in cancer and the development of novel mechanism-based cancer therapies. Silvio Gutkind on the web Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications More J Silvio Gutkind on LinkedIn Gutkind Lab on Twitter UCSD Moores Cancer Center Dr.